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Chemical Structure| 1210344-57-2 Chemical Structure| 1210344-57-2

Structure of Ertugliflozin
CAS No.: 1210344-57-2

Chemical Structure| 1210344-57-2

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PF-04971729 is a selective sodium-dependent glucose cotransporter (SGLT) inhibitor which selectively targets SGLT2.

Synonyms: PF-04971729; MK-8835

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Product Details of Ertugliflozin

CAS No. :1210344-57-2
Formula : C22H25ClO7
M.W : 436.88
SMILES Code : O[C@@H]1[C@](O2)(CO)CO[C@]2(C3=CC=C(Cl)C(CC4=CC=C(OCC)C=C4)=C3)[C@H](O)[C@H]1O
Synonyms :
PF-04971729; MK-8835
MDL No. :MFCD21609259
InChI Key :MCIACXAZCBVDEE-CUUWFGFTSA-N
Pubchem ID :44814423

Safety of Ertugliflozin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
C2C12 cells 10 μM Under hyperglycemic conditions, Ertugliflozin significantly increased the viability of C2C12 cells and inhibited hyperglycemia-induced cell death. Acta Pharmacol Sin. 2023 Jun;44(6):1161-1174
BV-2 microglia 10 or 20 µM 24 hours To evaluate the effect of Ertugliflozin on high glucose-induced inflammatory toxicity. Results showed that Ertugliflozin did not significantly inhibit BV-2 microglial proliferation or protect cells from high glucose-induced cytotoxicity. Biomedicines. 2023 Dec 22;12(1):36
human-umbilical-vein endothelial cells (HUVECs) 100 µM Investigate the effects of Ertugliflozin on mitochondrial oxidative phosphorylation and glucose uptake. Results showed no significant effect on OCR at 100 µM. Int J Mol Sci. 2022 Jul 19;23(14):7966
human-umbilical-vein endothelial cells (HUVECs) 10 µM Investigate the effects of Ertugliflozin on mitochondrial oxidative phosphorylation and glucose uptake. Results showed no significant effect on OCR at 10 µM. Int J Mol Sci. 2022 Jul 19;23(14):7966

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice High-fat, high-sucrose diet-induced diabetic cardiomyopathy Mixed with diet 0.5 mg/g diet For 4 months Evaluate the effects of Ertugliflozin on mitochondrial function, high-energy phosphates, and genes encoding mitochondrial proteins, preventing myocardial hypertrophy and diastolic dysfunction J Am Heart Assoc. 2021 Jul 6;10(13):e019995
Mice Gαq-overexpressing mice Oral 0.5 mg/g chow 16 weeks ERTU treatment prevented cardiac hypertrophy, dilation, contractile dysfunction, myocyte apoptosis, and interstitial fibrosis in Gαq mice, and improved mitochondrial function. J Mol Cell Cardiol Plus. 2025 Apr 9;12:100296
C57BL/6J mice High fat, high sucrose (HFHS) diet-induced diabetic cardiomyopathy (DCMP) model Dietary administration 0.5 mg/g of diet One month duration ERTU decreased myocardial intracellular sodium levels, improved energetics and contractile function Biomed Pharmacother. 2023 Apr;160:114310

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01948986 Renal Impairment|Type 2 Diabet... More >>es Mellitus Less << PHASE1 COMPLETED 2014-10-16 -
NCT04167761 Cardiovascular Diseases|Athero... More >>sclerosis|Type 2 Diabetes|Insulin Resistance Less << EARLY_PHASE1 COMPLETED 2023-12-31 Stanford University, Stanford,... More >> California, 94305, United States Less <<
NCT01127308 Type 2 Diabetes Mellitus (T2DM... More >>) Less << PHASE1 COMPLETED 2025-07-10 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.44mL

2.29mL

1.14mL

22.89mL

4.58mL

2.29mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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